Anticoagulant therapy

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  1. Dabigatran
    • oral direct thrombin inhibitor
    • metabolism: 80% renal, 20% hepatic
  2. Argatroban
    • parenteral direct thrombin inhibitor
    • approved for treatment of HIT
    • continuous IV infusion
    • short half life (1 hr)
    • APTT monitoring
    • metabolism: hepatic
  3. lepirudin and bivalirudin
    • parenteral direct thrombin inhibitor
    • approved for HIT
    • continuous IV infusion
    • short half life (1-2 hrs)
    • APTT monitoring
    • metabolism: renal
  4. rivaroxaban
    • direct factor Xa inhibitor
    • metabolism: mostly hepatic
  5. apixaban
    • direct factor Xa inhibitor
    • metabolism: mostly hepatic
  6. idarucizumab
    anti-dabigatran monoclonal antibody Fab
  7. andexanet
    inactive Xa analogue to neutralize factor Xa inhibitors
  8. Aspirin
    • anti-platelet¬†
    • irreversibly inhibits COX1/2, decreases synthesis of thromboxane A2 (potent platelet agonist)
    • inhibits platelet fn for the life of the platelet
    • adverse effects: bleeding, GI ulceration, allergy and bronchospasm, interstitial nephritis, papillary necrosis, proteinuria, renal failure, Reye's syndrome (rapidly progressive encephalopathy and hepatic dysfunction) in children with viral illness
  9. clopidogrel
    • thienopyridine
    • P2Y12 receptor antagonist (high affinity, essentially irreversible)
    • blocks activation of platelets by reducing ADP activation of P2Y12 receptor
    • oral
    • adverse effects: bleeding, GI irritation, thrombocytopenia, neutropenia
  10. triclopidine
    • thienopyridine
    • P2Y12 receptor antagonist (high affinity, essentially irreversible)
    • blocks activation of platelets by reducing ADP activation of P2Y12 receptor
    • oral
    • adverse effects: bleeding, GI irritation, thrombocytopenia, neutropenia
  11. prasugrel
    • thienopyridine
    • P2Y12 receptor antagonist (high affinity, essentially irreversible)
    • blocks activation of platelets by reducing ADP activation of P2Y12 receptor
    • oral
    • adverse effects: bleeding, GI irritation, thrombocytopenia, neutropenia
  12. ticagrelor
    • cyclopentyltriazolopyrimidine
    • P2Y12 receptor antagonist (noncompetitive inhibitor of P2Y12 - reversible)
    • blocks activation of platelets by reducing ADP activation of P2Y12 receptor
    • oral
    • adverse effects: bleeding, GI irritation, thrombocytopenia, neutropenia
  13. abciximab
    • Fab fragment of a monoclonal antibody
    • inhibits binding of fibrinogen to glycoprotein IIb/IIIa
    • adverse effects: bleeding, thrombocytopenia
  14. tirofiban
    • small molecule
    • inhibits binding of fibrinogen to glycoprotein IIb/IIIa
    • adverse effects: bleeding, thrombocytopenia
  15. eptifibitide
    • cyclic heptapeptide
    • inhibits binding of fibrinogen to glycoprotein IIb/IIIa
    • adverse effects: bleeding, thrombocytopenia
  16. dipyridamole
    • multiple mechanisms: stimulates prostacyclin synthesis, inhibits adenosine deaminase and phosphodiesterase
    • vasodilatory effects on blood vessels
    • oral or IV
    • adverse effects: headache
    • often used in combination with aspirin
  17. streptokinase
    • fibrinolytic agent
    • single chain polypeptide derived from beta-hemolytic streptococcus
    • binds to plasminogen, forming a complex that becomes allosterically active, allowing the streptokinase/plasminogen complex to generate plasmin
    • IV or catheter-directed
    • not fibrin specific (also cleaves fibrinogen)
    • adverse effects: bleeding, allergic rxns, hypotension
  18. urokinase (u-PA)
    • fibrinolytic agent
    • isolated from human urine or kidney cells
    • protease that directly cleaves plasminogen to form plasmin
    • non-antigenic
    • IV
    • not fibrin specific: also cleaves fibrinogen
    • adverse effects: bleeding
  19. tissue plasminogen activator (t-PA)
    • recombinant t-PA (alteplase, reteplase, tenecteplase)
    • proteases that directly cleaves plasminogen to form plasmin
    • relative fibrin-specific (does not cleave fibrinogen, resulting in more localized, rather than systemic fibrinolytic activity)
    • short half life (minutes) - must be used in conjunction with heparin
    • non-antigenic
    • IV
    • adverse effects: bleeding

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Author:
jboi
ID:
319067
Filename:
Anticoagulant therapy
Updated:
2016-04-18 02:18:11
Tags:
anticoagulants
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Description:
MOHD 3
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